LUF6096 是一种有效的腺苷 A3 受体 (adeNOSine A3 receptor) 变构增强剂。LUF6096 对任何腺苷受体显示出低正构亲和力。LUF6096 在心肌缺血/再灌注损伤中显示出保护作用。
产品描述
LUF6096 is a potent allosteric enhancer of the adenosine A3 receptor. LUF6096 is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury.
体外活性
LUF6096 (10 μM; 30-120 min) decreases the dissociation rate of 125I-AB-MECA from the A3 receptor by 2.5 times in CHO cell membranes. LUF6096 (10 μM; pretreated for 15 min) significantly enhances the intrinsic activity of Cl-IB-MECA for the inhibition of the forskolin-stimulated cAMP production in CHO cells[1].
体内活性
LUF6096 (twice i.v. bolus for 0.5 mg/kg or single i.v. bolus for 1 mg/kg) protects against myocardial ischemia/reperfusion injury in dogs[1].
Cas No.
1116652-18-6
分子式
C22H21Cl2N3O
分子量
414.33
别名
CF-602
储存和溶解度
DMSO:18mg/mL (43.5mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years